Lestaurtinib (1 mg)

126565

JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB

439.46

(9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one

Potent JAK2, FLT3 and TrkA inhibitor (IC₅₀ values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC₅₀ values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC₅₀ = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC₅₀ = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.

≥98% (HPLC)

Soluble to 100 mM in DMSO and to 25 mM in ethanol

CEP-701

O=C(NC3)C1=C3C(C4=CC=CC=C4N5[C@@]78C)=C5C2=C1C6=C(C=CC=C6)N2[C@](O7)(C[C@](CO)8O)[H]

C₂₆H₂₁N₃O₄

111358-88-4